Zafirlukast
- Atc Codes:R03DC01
- CAS Codes:107753-78-6
- PHARMGKB ID:107753-78-6
Table of contents
- Brand Names
- Chemistry
- Pharmacologic Category
- Mechanism of Action
- Therapeutic Use
- Pregnancy and Lactation Implications
- Contraindications
- Warnings and Precautions
- Adverse Reactions
- Caution and personalized dose adjustment in patients with the following genotypes
- Other genes that may be involved
- Substrate of
- Inhibits
- Drug Interactions
- Dosage
- Pharmacokinetics and Pharmacodynamics
- Special Considerations
Brand Names
Europe
Belgium: Accolate, Resma; Czech Republic: Accolate; Finland: Accolate; Hungary: Accolate; Ireland: Accolate; Italy: Accoleit, Zarfist; Luxembourg: Accolate; Netherlands: Accolate; Poland: Accolate; Portugal: Accolate; Slovakia: Accolate; Slovenia: Accolate; Spain: Accolate, Aeronix, Olmorán; UK: Accolate.
North America
Canada: Accolate; USA: Accolate.
Latin America
Argentina: Accolate; Brazil: Accolate; Mexico: Accolate.
Asia
Japan: Accolate.
Drug combinations
Chemistry
Zafirlukast: C~31~H~33~N~3~O~6~S. Mw: 575.68. (1) Carbamic acid, [3-[[2-methoxy-4-[[[2-methylphenyl)sulfonyl]amino]carbonyl]phenyl]methyl]-1-methyl-1H-indol-5-yl]-, cyclopentyl ester; (2) Cyclopentyl 3-[2-methoxy-4-[(o-tolylsulfonyl)carbamoyl]benzyl]-1-methylindole-5-carbamate. CAS-107753-78-6 (1995).
Pharmacologic Category
Anti-inflammatory Agents; Leukotriene Modifiers. (ATC-Code: R03DC01).
Mechanism of action
A selective and competitive leukotriene-receptor antagonist of leukotriene D~4~ and E~4~ (LTD4 and LTE4), components of slow-reacting substance of anaphylaxis (SRS-A).
Therapeutic use
Prophylaxis and chronic treatment of asthma in adults and children ≥5 years of age.
Pregnancy and lactiation implications
Fetal defects observed when administered in maternally toxic doses. Contraindicated in nursing women, due to tumorigenicity observed in animal studies.
Unlabeled use
Contraindications
Hypersensitivity to zafirlukast or any component of the formulation.
Warnings and precautions
In rare cases, patients may present with systemic eosinophilia, sometimes presenting with clinical features of vasculitis consistent with Churg-Strauss syndrome. Reports exist of hepatic adverse events (including hepatitis, hyperbilirubinemia, and hepatic failure); female patients may be at greater risk. Use caution in alcoholic cirrhosis (clearance reduced). An increased proportion of patients >55 years of age reported infections as compared to placebo-treated patients (predominantly affected respiratory tract; associated with co-administration of inhaled corticosteroids). Not FDA approved for use in reversal of bronchospasm in acute asthma attacks, including status asthmaticus. Reports of agranulocytosis in association with zafirlukast.